Atazanavir sulfate, also known as (3S,8S,9S,12S)-3,12-Bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,6,10,13-pentaazatetradecanedioic acid dimethyl ester, sulfate, prevents the formation of mature HIV virions in HIV-1 infected cells by selectively inhibiting the virus-specific processing of certain polyproteins (viral Gag and Gag-Pol). Atazanavir sulfate is currently approved for the treatment of HIV infection.
Atazanavir is contraindicated for coadministration with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. Due to inhibition effects of atazanavir on CYP3A, CYP2C8, and UGT1A1, caution is advised when prescribing drugs primarily metabolized by CYP3A, CYP2C8, or UGT1A1 for patients receiving atazanavir. Common adverse events associated with atazanavir include hyperbilirubinemia, rash, nausea, headache, and jaundice/scleral icterus. Adverse events experienced by some patients and for which a causal relationship has not been established include diabetes mellitus/hyperglycemia, PR interval prolongation, hemophilia, and fat redistribution.
Despite the beneficial activities of atazanavir, there is a continuing need for new compounds to treat the aforementioned diseases and conditions.